Aniracetam (Draganon, Sarpul, Ampamet, Memodrin, Referan) is also known as 1-[(4-methoxyphenyl)carbonyl]pyrrolidin-2-one.

It is classified both as a Racetam and an Ampakine nootropic substance with interactions with the cholinergic, dopaminergic, serotonergic and glutamatergic systems.

Aniracetam is a lipophilic derivative of Piracetam, exhibiting many of the same same effects with an estimated 3-6x increased potency. It increases cholinergic neurotransmission as is typical of the Racetam class of nootropics.

It also positively modulates glutamatergic activity via AMPA receptors and is considered the model for Ampakine agents. Additional mechanisms of action involve Dopaminergic, Serotonergic and GABAergic pathways.

Like Piracetam, it is hypothesized to facilitate cholinergic transmission. Unlike Piracetam, Aniracetam is fat-soluble which may contribute to its increased potency. [1]

Aniracetam is also a positive modulator of metabotropic gultamate receptors and alpha-amino-3-hydroxy-5-methyl-4-isoxazolepropionic AMPA excitatory receptors.

It is considered to be the first AMPAkine compound invented and is the prototype for other Ampakines that have followed.

Aniracetam Chemical Structure

Like Piracetam, Aniracetam has a 2-pyrrolidinone nucleus which is the distinctive feature of the Racetam family of compounds.

However, where Piracetam has an amine group, Aniracetam has a methylated phenyl group. This modification gives Aniracetam greater fat solubility which results in a potency between 3 – 6 times greater than Piracetam.

Pharmacokinetics

Oral Bio-availability was between 8.6 – 11.4% in rats when consumed on an empty stomach. [3]

Given its lipophilic nature, bio-availability should be improved when consumed with fatty acids, however no studies are available that examine this.

Serum levels of Aniracetam peak at 2.3mcg/L with a 300mg dosage and 14.1mcg/L following a 1200mg dose. It has a Cmax of 8.75+/-7.82 and 8.65+/-8.7ng/mL and a Tmax of 0.4+/-0.1 following a 400 mg dosage. [4]

The elimination half-life of Aniracetam is a rapid 35 minutes following oral ingestion. Within 48 hours of administration, 84% of the dosage was eliminated in urine, 0.8% in feces and 11% was expelled as carbon dioxide. [1]

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Metabolites

There is a high degree of first pass hepatic metabolism into the metabolites 2-pyrrolidinone, N-anisoyl-GABA, and anisic acid.

N-anisoyl-GABA is the primary metabolite, making up 70% by weight of the initial dosage following transformation by the liver. [4]

A study on the attentional and vigilance task performance of rats given Aniracetam found that 2-pyrrolidinone and N-anisoyl-GABA are the main active metabolites.

Both of these compounds partially mimicked the effects of Aniracetam in improving 8-OHDPAT-induced attentional and vigilance impairments. [8]

Aniracetam Mechanisms of Action

The mechanism of action for Aniracetam is not fully understood, however trials have shown it to exhibit cholinergic, dopaminergic, serotonergic, glutamatergic and indirect adrenergic effects.

Like Piracetam and other Racetam nootropics, Aniracetam is a positive modulator of Nicotinic receptors for the neurotransmitter acetylcholine.

In animal studies, it alleviates memory and learning impairments caused by cholinergic antagonists.

It is also observed to increase acetylcholine release from the hippocampus in rat trials and facilitates an increase in cholinergic neurotransmission. [36]

AMPA Glutamatergic Receptors

Aniracetam is a positive allosteric modulator of alpha-amino-3-hydroxy-5-methylisoxazole-4-propionic acid (AMPA, quisqualate) receptors for the neurotransmitter Glutamate.

These neuro-receptors mediate fast synaptic transmission in the central nervous system and are integral to synaptic plasticity and Long-Term Potentiation by which memories are stored.

Aniracetam binds to non-active AMPA receptors and modifies them so they exhibit a reduced rate of desensitization. This results in a greater level of activation when Glutamate or other agonists are present.

Aniracetam is also a positive modulator of kainate Glutamatergic receptors but does not directly influence NMDA receptors. [15]

GABAergic Receptors

Aniracetam has been observed to enhance cortical GABAergic inhibition. It was found to increase the total charge of Inhibitory Post-Synaptic Currents (IPSC’s).

Serotonergic Receptors

Turnover is a measure of the amount and rate at which a neurotransmitter is transmitted across the synaptic cleft and re-synthesized within the pre-synaptic neuron.

An increased rate of turnover means that more of a neurotransmitter is being used while a decreased rate means that less is being used.

Aniracetam administered at 50 mg/kg was found to delay Serotonin (5-HT) turnover in the hypothalamus and increase 5-HT turnover in the cortex, striatum and stem. [6]

Dopaminergic Receptors

Aniracetam at 50 mg/kg reduced Dopamine turnover rates in the striatum. It further reduced dopamine levels in the striatum and hypothalamus.

In another study, Aniracetam was found to facilitate dopaminergic signalling via dopamine release and dopamine D2 receptor activation through stimulation of excitatory nicotinic acetylcholine receptors. [6]

Adrenergic Receptors

Indirectly, Aniracetam is observed to increase [3H]noradrenaline (norepinephrine) release in the rat hippocampus.

This is mediated by Aniracetam’s effects on AMPA receptors which leads to enhanced noradrenaline (norepinephrine) secretions from neurons. The result is a slight stimulatory effect on the Central Nervous System.

This effect is only observed in larger dosages of Aniracetam yielding high micromolar concentrations of at least 100µM. [20]

Aniracetam for Cognitive Enhancement

Aniracetam was found to improve cognitive function in elderly patients diagnosed with mild to moderate impairments caused by senile dementia of the Alzheimer type (SDAT). [1]

It decreased the rate of ionotropic AMPA receptor desensitization in the hippocampus, leading to enhanced glutamatergic signalling.

It also increased EPSPs in the fibre-CA3 synapses suggesting a mechanism for improved memory formation. [17]

Ampakine nootropics in general have been found to increase levels of Brain-derived Neurotrophic factor (BDNF) in entorhinal/hippocampal slices.

This protein is integral to the maintenance, growth and development of new neurons leading to improved neuroplasticity and memory function.

Ampakine-induced upregulation is attributed to AMPA receptor agonists and was not reversed when an NMDA receptor antagonist was administered. [29]

Neuroprotection

Aniracetam reverses some forms of cognitive damage caused by prenatal alcohol exposure. [35] It can also protect the brain against damage caused by electroconvulsive shock and cerebral ischaemia. [1]

It is shown to reduce impairments caused by cerebrovascular disorders and defects.

In patients with cognitive deficits caused by cerebrovascular disease, a 1000mg/day Aniracetam dosage for 1 month and a 1500mg/day dosage for 4 months were both found to be more effective than a placebo at reducing impairments. [1]

A 1500mg dosage of Aniracetam also reduced scopolamine-induced cognitive impairments in healthy young individuals. It was found to be more effective than a 2400mg dosage of Piracetam on the same model. [23, 1]

Anxiolytic and Anti-Depressant Properties

Aniracetam is observed to improve anxiety in rats leading to an increase in social interactions.

This anxiolytic effect was observed between dosages of 10mg/kg to 100mg/kg of bodyweight. It has also been found to reduce impulsiveness in rat behavior. [24]

Aniracetam also exhibits an anti-depressant effect in aged (25-30 months old) rats as measured by reduced immobility times in a forced swim test. This result was not repeated in trials with younger (9 week old) rats.

This effect is attributed to its metabolites 2-pyrrolidinone and N-anisoyl-GABA which lead to increased dopaminergic transmission via stimulation of nicotinic acetylcholine receptors. [25]

Aniracetam Safety and Side Effects

Aniracetam shows a high degree of tolerability with no detected liver toxicity. No increases in liver enzymes have been observed following hepatic Aniracetam metabolism.

Human trials are limited and there have not been any established rates of incidents for serious adverse effects.

Mild side effects have been reported consisting of restlessness, anxiety, and sleeplessness. Less common side effects include “headache, somnolence, vertigo, mild epigastric pain, nausea, diarrhoea and rash.” [1]

Dosage and Administration

Oral Aniracetam administration has been studied at dosages between 600mg per day to 1500mg per day.

Patients with Senile Dementia of the Alzheimer’s Type (SDAT) are treated at 1000mg to 1500mg per day taken as a single dose or as two 750mg oral tablets per day.

In Japan, dosages of 200mg taken three times a day is recommended for patients with anxiety or depression symptoms following a cerebral infarction. [1]

In rats administered ethanol (alcohol) at 4 g/kg/24 h; 38% v/v throughout the pregnancy, severe cognitive disabilities developed in the offspring.

Administering 50 mg/kg Aniracetam dosages for 10 days after birth starting on the 18th day lead to a reversal of cognitive deficits. The improvements were mediated through post-natal modulation of AMPA receptors in the hippocampal CA-1 pyramidal cells. [35]

Lee CR, Benfield P. Aniracetam. An overview of its pharmacodynamic and pharmacokinetic properties, and a review of its therapeutic potential in senile cognitive disorders. Drugs Aging. 1994 Mar;4(3):257-73.

Aniracetam was found to benefit elderly patients with mild to moderate cognitive impairment caused by senile dementia of the Alzheimer type.

Dosages of 1500mg/day for 4 and 6 months were significantly more effective than a placebo at improving cognitive function as measured by a battery of 18 tests.

Aniracetam 1500 mg performed better than the placebo in 18 of 18 tests and performed better than 2400mg/day of Piracetam in 8 of 18 tests in a 6 month trial.

The study found that Aniracetam is well tolerated and does not result in an increase in liver enzyme levels. [1]

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